《Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models》 was written by Romussi, Alessia; Cappa, Anna; Vianello, Paola; Brambillasca, Silvia; Cera, Maria Rosaria; Dal Zuffo, Roberto; Faga, Giovanni; Fattori, Raimondo; Moretti, Loris; Trifiro, Paolo; Villa, Manuela; Vultaggio, Stefania; Cecatiello, Valentina; Pasqualato, Sebastiano; Dondio, Giulio; So, Chi Wai Eric; Minucci, Saverio; Sartori, Luca; Varasi, Mario; Mercurio, Ciro. HPLC of Formula: 109384-19-2 And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:
Lysine-specific demethylase 1 (LSD1 or KDM1A) is a FAD-dependent enzyme that acts as a transcription corepressor or coactivator by regulating the methylation status of histone H3 lysines K4 and K9, resp. KDM1A represents an attractive target for cancer therapy. While, in the past, the main medicinal chem. strategy toward KDM1A inhibition was based on the optimization of ligands that irreversibly bind the FAD cofactor within the enzyme catalytic site, we and others have also identified reversible inhibitors. Herein we reported the discovery of 5-imidazolylthieno[3,2-b]pyrroles, a new series of KDM1A inhibitors endowed with picomolar inhibitory potency, active in cells and efficacious after oral administration in murine leukemia models. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2HPLC of Formula: 109384-19-2)
tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.HPLC of Formula: 109384-19-2
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem